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Sulfonium, an Underestimated Moiety for Structural Modification, Alters the Antibacterial Profile of Vancomycin Against Multidrug-Resistant Bacteria

文献类型：期刊论文

作者Guan, Dongliang1,2; Chen, Feifei3; Qiu, Yunguang1,2; Jiang, Bofeng1; Gong, Likun2,3; Lan, Lefu2,3; Huang, Wei1,2
刊名ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
出版日期2019-05-13
卷号58期号:20页码:6678-6682
关键词antibacterial multidrug-resistant bacteria sulfonium vancomycin
ISSN号1433-7851
DOI10.1002/anie.201902210
通讯作者Lan, Lefu(llan@simm.ac.cn) ; Huang, Wei(huangwei@simm.ac.cn)
英文摘要In the antibiotics arsenal, vancomycin is a last resort for the treatment of intractable infections. However, this situation is under threat because of the increasing appearance of vancomycin-resistant bacteria (VRB). Herein, we report a series of novel vancomycin derivatives carrying a sulfonium moiety. The sulfonium-vancomycin derivatives exhibited enhanced antibacterial activity against VRB both invitro and invivo. These derivatives also exhibited activity against some Gram-negative bacteria. The sulfonium modification enhanced the interaction of vancomycin with the bacterial cell membrane and disrupts membrane integrity. Furthermore, the invivo pharmacokinetic profile, stability, and toxicity of these derivatives demonstrated good druggability of the sulfonium-vancomycin analogues. This work provides a promising strategy for combating drug-resistant bacterial infection, and advances the knowledge on sulfonium derivatives for structural optimization and drug development.
WOS关键词ALA-D-LAC ; ANTIMICROBIAL RESISTANCE ; STAPHYLOCOCCUS-AUREUS ; GLYCOPEPTIDE ; LIPOGLYCOPEPTIDE ; ORITAVANCIN ; ANALOGS ; TELAVANCIN ; STRATEGY ; DISEASE
资助项目National Natural Science Foundation of China (NNSFC)[21572244] ; National Natural Science Foundation of China (NNSFC)[21877116] ; National Natural Science Foundation of China (NNSFC)[31700124] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program of China[2018ZX09711002-006] ; Youth Innovation Promotion Association of CAS[2017328]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000471977400032
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/289454]  
专题新药研究国家重点实验室
通讯作者Lan, Lefu; Huang, Wei
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Biotherapeut Discovery Res, CAS Key Lab Receptor Res,CAS Ctr Excellence Mol C, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Guan, Dongliang,Chen, Feifei,Qiu, Yunguang,et al. Sulfonium, an Underestimated Moiety for Structural Modification, Alters the Antibacterial Profile of Vancomycin Against Multidrug-Resistant Bacteria[J]. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION,2019,58(20):6678-6682.
APA Guan, Dongliang.,Chen, Feifei.,Qiu, Yunguang.,Jiang, Bofeng.,Gong, Likun.,...&Huang, Wei.(2019).Sulfonium, an Underestimated Moiety for Structural Modification, Alters the Antibacterial Profile of Vancomycin Against Multidrug-Resistant Bacteria.ANGEWANDTE CHEMIE-INTERNATIONAL EDITION,58(20),6678-6682.
MLA Guan, Dongliang,et al."Sulfonium, an Underestimated Moiety for Structural Modification, Alters the Antibacterial Profile of Vancomycin Against Multidrug-Resistant Bacteria".ANGEWANDTE CHEMIE-INTERNATIONAL EDITION 58.20(2019):6678-6682.

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来源：上海药物研究所

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